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A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability.
Payne CE, Brown AR, Theile JW, Loucif AJ, Alexandrou AJ, Fuller MD, Mahoney JH, Antonio BM, Gerlach AC, Printzenhoff DM, Prime RL, Stockbridge G, Kirkup AJ, Bannon AW, England S, Chapman ML, Bagal S, Roeloffs R, Anand U, Anand P, Bungay PJ, Kemp M, Butt RP, Stevens EB. Payne CE, et al. Among authors: printzenhoff dm. Br J Pharmacol. 2015 May;172(10):2654-70. doi: 10.1111/bph.13092. Epub 2015 Apr 10. Br J Pharmacol. 2015. PMID: 25625641 Free PMC article.
Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels.
McCormack K, Santos S, Chapman ML, Krafte DS, Marron BE, West CW, Krambis MJ, Antonio BM, Zellmer SG, Printzenhoff D, Padilla KM, Lin Z, Wagoner PK, Swain NA, Stupple PA, de Groot M, Butt RP, Castle NA. McCormack K, et al. Proc Natl Acad Sci U S A. 2013 Jul 16;110(29):E2724-32. doi: 10.1073/pnas.1220844110. Epub 2013 Jul 1. Proc Natl Acad Sci U S A. 2013. PMID: 23818614 Free PMC article.
Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release.
Alexandrou AJ, Brown AR, Chapman ML, Estacion M, Turner J, Mis MA, Wilbrey A, Payne EC, Gutteridge A, Cox PJ, Doyle R, Printzenhoff D, Lin Z, Marron BE, West C, Swain NA, Storer RI, Stupple PA, Castle NA, Hounshell JA, Rivara M, Randall A, Dib-Hajj SD, Krafte D, Waxman SG, Patel MK, Butt RP, Stevens EB. Alexandrou AJ, et al. PLoS One. 2016 Apr 6;11(4):e0152405. doi: 10.1371/journal.pone.0152405. eCollection 2016. PLoS One. 2016. PMID: 27050761 Free PMC article.
Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes.
Storer RI, Pike A, Swain NA, Alexandrou AJ, Bechle BM, Blakemore DC, Brown AD, Castle NA, Corbett MS, Flanagan NJ, Fengas D, Johnson MS, Jones LH, Marron BE, Payne CE, Printzenhoff D, Rawson DJ, Rose CR, Ryckmans T, Sun J, Theile JW, Torella R, Tseng E, Warmus JS. Storer RI, et al. Bioorg Med Chem Lett. 2017 Nov 1;27(21):4805-4811. doi: 10.1016/j.bmcl.2017.09.056. Epub 2017 Sep 28. Bioorg Med Chem Lett. 2017. PMID: 29029933
Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7.
Swain NA, Batchelor D, Beaudoin S, Bechle BM, Bradley PA, Brown AD, Brown B, Butcher KJ, Butt RP, Chapman ML, Denton S, Ellis D, Galan SRG, Gaulier SM, Greener BS, de Groot MJ, Glossop MS, Gurrell IK, Hannam J, Johnson MS, Lin Z, Markworth CJ, Marron BE, Millan DS, Nakagawa S, Pike A, Printzenhoff D, Rawson DJ, Ransley SJ, Reister SM, Sasaki K, Storer RI, Stupple PA, West CW. Swain NA, et al. J Med Chem. 2017 Aug 24;60(16):7029-7042. doi: 10.1021/acs.jmedchem.7b00598. Epub 2017 Aug 10. J Med Chem. 2017. PMID: 28682065
The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics.
Pryde DC, Swain NA, Stupple PA, West CW, Marron B, Markworth CJ, Printzenhoff D, Lin Z, Cox PJ, Suzuki R, McMurray S, Waldron GJ, Payne CE, Warmus JS, Chapman ML. Pryde DC, et al. Medchemcomm. 2017 Apr 28;8(6):1255-1267. doi: 10.1039/c7md00131b. eCollection 2017 Jun 1. Medchemcomm. 2017. PMID: 30108836 Free PMC article.
In vitro and in vivo characterization of a novel naphthylamide ATP-sensitive K+ channel opener, A-151892.
Gopalakrishnan M, Buckner SA, Shieh CC, Fey T, Fabiyi A, Whiteaker KL, Davis-Taber R, Milicic I, Daza AV, Scott VE, Castle NA, Printzenhoff D, London B, Turner SC, Carroll WA, Sullivan JP, Coghlan MJ, Brune ME. Gopalakrishnan M, et al. Br J Pharmacol. 2004 Sep;143(1):81-90. doi: 10.1038/sj.bjp.0705908. Epub 2004 Aug 9. Br J Pharmacol. 2004. PMID: 15302680 Free PMC article.
13 results